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QNZ (EVP4593)

Catalog No.
A4217
Potent NF-κB inhibitor
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$70.00
In stock
5mg
$65.00
In stock
25mg
$260.00
In stock

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Email: [email protected]

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Background

EVP4593 is an inhibitor of NF-κB pathway with IC50 value of 11nM [1].

EVP4593 is a quinazoline derivative. It is screened out from a luciferase reporter gene-based assay using human Jurkat T cells. EVP4593 is found as an inhibitor of PMA/PHA-induced NF-κB pathway. It shows significant inhibition of both NF-κB transcriptional activation and TNF-α production (IC50 value of 7nM). Additionally, EVP4593 also has anti-inflammatory efficacy. It inhibits edema formation in a rat carrageenin-induced paw edema model [1].

Since NF-κB pathway may play a direct role in Huntington’s disease (HD) pathogenesis, EVP4593 is found to have beneficial effects in Drosophila HD transgenic model. It significantly slows the progressive decline in the climbing speed without toxic effects [2].

References:
[1] Tobe M, Isobe Y, Tomizawa H, Nagasaki T, Takahashi H, Fukazawa T, Hayashi H. Discovery of quinazolines as a novel structural class of potent inhibitors of NF-kappa B activation. Bioorg Med Chem. 2003 Feb 6;11(3):383-91.
[2] Wu J, Shih HP, Vigont V, Hrdlicka L, Diggins L, Singh C, Mahoney M, Chesworth R, Shapiro G, Zimina O, Chen X, Wu Q, Glushankova L, Ahlijanian M, Koenig G, Mozhayeva GN, Kaznacheyeva E, Bezprozvanny. Neuronal store-operated calcium entry pathway as a novel therapeutic target for Huntington's disease treatment. Chem Biol. 2011 Jun 24;18(6):777-93.

Product Citation

Chemical Properties

StorageStore at -20°C
M.Wt356.42
Cas No.545380-34-5
FormulaC22H20N4O
Solubility≥15.05 mg/mL in DMSO, ≥10.06 mg/mL in EtOH with ultrasonic,insoluble in H2O
Chemical Name4-N-[2-(4-phenoxyphenyl)ethyl]quinazoline-4,6-diamine
SDFDownload SDF
Canonical SMILESC1=CC=C(C=C1)OC2=CC=C(C=C2)CCNC3=NC=NC4=C3C=C(C=C4)N
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Protocol

Cell experiment [1]:

Cell lines

YAC128 medium spiny neurons primary cultures

Preparation method

The solubility of this compound in DMSO is >15.05mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

300 nM

Applications

In YAC128 MSN neurons, the main locus of pathology in HD (Huntington’s disease), EVP4593 (300 nM) resulted in strong attenuation of Store-operated Ca2+ entry (SOC) influx.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1] Wu J, Shih H P, Vigont V, et al. Neuronal store-operated calcium entry pathway as a novel therapeutic target for Huntington's disease treatment[J]. Chemistry & biology, 2011, 18(6): 777-793.

Biological Activity

Description QNZ is an inhibitor of NF-κB with IC50 value of 11 nM in human Jurkat cells.
Targets NF-κB          
IC50 11 nM (in human Jurkat cell line)          

Quality Control

Chemical structure

QNZ (EVP4593)

Related Biological Data

QNZ (EVP4593)

Related Biological Data

QNZ (EVP4593)